[4-(HETEROARYL)PIPERAZINE-1-YL]-(2,5-SUBSTITUTED PHENYL)METHANONE DERIVATIVES AS GLYCINE-1 (GLYT-1) CARRIER INHIBITORS FOR TREATING NEUROLOGIC AND PSYCHONEUROLOGICAL DISEASES Russian patent published in 2010 - IPC C07D417/04 C07D417/14 A61K31/496 A61K31/5377 A61P25/00 

FIELD: medicine, pharmaceutics.

SUBSTANCE: present invention refers to compounds of general formula I and to their pharmaceutically acceptable acid addition salts. The compounds of the present invention exhibit the properties of glycine carrier 1 (GlyT-1) inhibitors. In formula I , R¹ represents -OR^1', -SR^1' or morpholinyl; R^1' represents lower alkyl, halogen-substituted lower alkyl, or represents -(CH₂)_n-lower cycloalkyl; R² represents -S(O)₂-lower alkyl, -S(O)₂NH-lower alkyl, NO₂ or CN; X¹ represents CR³ or N; X² represents CR^3' or N; R³/R^3' independently represent hydrogen, halogen, lower alkyl, CN, NO₂, -S(O)₂-phenyl, -S(O)₂-lower alkyl, -S(O)₂-pyridine-2, 3 or 4-yl, phenyl optionally substituted with one or two substitutes specified from the group consisting of NO₂ or halogen, or represent halogen-substituted lower alkyl, or represent -C(O)-lower alkyl; n has a value of 0, 1 or 2. The invention also concerns a drug containing one or more compounds of the invention and pharmaceutically appropriate excipients.

EFFECT: preparation of the compounds exhibiting the properties of glycine carrier inhibitors.

20 cl, 1 tbl, 133 ex